1. (A) Illustration depicting two types of pharmacokinetic instability of an ADC. Conjugating an antibody with drug can accelerate its clearance (green versus blue line).
(A) Illustration depicting two types of pharmacokinetic instability of an ADC. Conjugating an antibody with drug can accelerate its clearance (green versus blue line). Loss of drug from the ADC during circulation results in less drugged antibody relative to total antibody (blue versus black line). (B) Conceptualized relationship between drug antibody ratio (DAR), antitumor activity (efficacy), and elimination of antibody from blood (clearance). Excessive drugging can lead to a loss of efficacy due to reduced ADC exposure.
Paul Polakis Pharmacol Rev 2016;68:3-19
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